Synthesis and SAR of 4-(benzylideneamino)benzenesulfonamides as selective COX-2 inhibitors

MEDI 282

Shwu-Jiuan Lin, shwu-lin@tmu.edu.tw, Department of Medicinal Chemistry, College of Pharmacy, Taipei Medical University, 250 Wu-Hsing St., Taipei, 110, Taiwan and Li-Ming Yang, lmyang@nricm.edu.tw, Division of Medicinal Chemistry, National Research Institute of Chinese Medicine, 155-1, Li-Nong St., Sec. 2, Taipei, 112, Taiwan.
Nonsteroidal antiinflammatory drugs (NSAIDs) are widely used to treat pain, fever and inflammation. COX-2 selective inhibitors have proven to be effective anti-inflammatory and analgesic medicines with lower bleeding and ulcerogenic effects than traditional NSAIDs, which nonselectively inhibit COX-2 and COX-1. Recently, rofecoxib and valdecoxib has been withdrawn from the market due to the increased risk of heart attack and stroke. Thus, it is highly desirable to develop new selective COX-2 inhibitors to prevent the cardiovascular side effects. In the present study, a series of 4-(benzylideneamino)benzenesulfonamide derivatives was designed and synthesized for the evaluation as selective COX-2 inhibitors in a cellular assay using human whole blood. The design, synthesis and SAR among these compounds will be presented and discussed.
 

Poster Session
7:00 PM-9:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster

Division of Medicinal Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007